GPV0057 (Compound 5d) is a selective and potent P-glycoprotein ( P-gp ) inhibitor. GPV0057 is also a selective potassium channel K ir 2.1 activator. GPV0057 competitively binds to the substrate-binding site of P-gp, inhibiting ATP-dependent drug efflux to reverse multidrug resistance in tumor cells. GPV0057 can also stabilizes the open state of K ir 2.1 and promotes potassium ion influx. GPV0057 is promising for research of tumors with high P-gp expression, K ir 2.1-deficient diseases such as heart failure and Andersen-Tawil Syndrome.
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